5-HT Receptor Agonist

5-HT Receptor Agonists (409):

Cat. No.	Product Name	Effect	Purity

HY-B0189B

Mosapride citrate dihydrate	Agonist
Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine₄ receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC₅₀ values of 15.2 μM. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo.

HY-B0121BS

Sumatriptan-d₆ succinate	Agonist	99.63%
Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with K_is of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research.

HY-14848A

Naluzotan hydrochloride	Agonist	99.63%
Naluzotan hydrochloride is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC₅₀ and K_i of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K⁺ channel blocker, with IC₅₀ of 3800 nM.

HY-14547A

Bifeprunox mesylate	Agonist	99.89%
Bifeprunox mesylate is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pK_is of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC₅₀ of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox mesylate is an antipsychotic for the research of schizophrenia.

HY-110094

BIMU 8	Agonist	≥99.0%
BIMU 8 is a potent and selective 5-HT4 agonist with EC₅₀s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors.

HY-160921

Capeserod	Agonist	98.66%
Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a K_i of 0.6 nM for 5-HT₄ receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models.

HY-160887

FPT	Agonist	98.06%
FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT_1AR, a full agonist at 5-HT_1BR and 5-HT_1DR with EC₅₀s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT₇R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models.

HY-18137

PF-04995274	Agonist	99.95%
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT₄R) agonist. PF-04995274 has an EC₅₀ range of 0.26-0.47 nM for human 5-HT_4A/4B/4D/4E (K_i range of 0.15-0.46 nM), and has an EC₅₀ range of 0.59-0.65 nM for rat 5-HT_4S/4L/4E (K_i of 0.30 nM for rat 5-HT_4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.

HY-103105A

LP 12 hydrochloride hydrate	Agonist	≥99.0%
LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a K_i of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (K_i values are 224 nM, 60.9 nM and >1000 nM, respectively).

HY-19134

EMD 56551	Agonist
EMD 56551 is a potent and selective 5-HT1A receptor agonist. EMD 56551 exerts anxiolytic activity.

HY-102057

Felcisetrag	Agonist	99.94%
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT₄ receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pK_i =9.4) for human 5-HT_4(c) receptors.

HY-B0716S1

Urapidil-d₃	Agonist	99.93%
Urapidil-d₃ is the deuterium labeled Urapidil. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.

HY-110024

S-14506 hydrochloride	Agonist	99.92%
S-14506 hydrochloride is a potent 5-HT1A agonist, as well as 5-HT_2A/2C antagonist. S-14506 hydrochloride displays dopamine antagonist properties by blocking dopamine D2 receptors. S-14506 hydrochloride inhibits the in vivo binding of [3H]raclopride in striatum and olfactory bulbs. S-14506 hydrochloride has the potential for the research of anxiolytic agent.

HY-156532C

(-)-5-HT2C agonist-3	Agonist
(-)-5-HT2C agonist-3 (compound (–)-19) is a 5-HT_2C selective agonist with G_q signaling preference, with EC₅₀ values ??for 5-HT₂ receptors of 5-HT_2C: 103 nM; 5-HT_2B: 570 nM; 5-HT_2A: 72 nM. (-)-5-HT2C agonist-3 can be used in antipsychotic research.

HY-116594

OPC-14523 free base	Agonist
OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC₅₀=47/56 nM), the 5-HT1A receptor (IC₅₀=2.3 nM), and the 5-HT transporter (IC₅₀=80 nM). OPC-14523 free base shows antidepressant-like activity.

HY-12959

Repinotan	Agonist
Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with K_i values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects.

HY-135555

5-Carboxamidotryptamine	Agonist	98.74%
5-Carboxamidotryptamine (5-CT) is a 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_5A, 5-HT₇ receptor agonist. 5-Carboxamidotryptamine has a K_i value of 4.6 nM for cloned human 5-HT_5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice.

HY-14441

ML 10302	Agonist	98.95%
ML 10302 is a potent agonist 5-HT4 receptor with K_i of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases.

HY-103108

CJ033466	Agonist	98.29%
CJ033466 is a novel and selective 5-HT₄ receptor partial agonist with an EC₅₀ of 9 nM and has gastroprokinetic effect.

HY-113008AS

cis-Urocanic acid-¹³C₃	Agonist	99.46%
cis-Urocanic acid-¹³C₃ is the ¹³C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor[1].

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